1. Signaling Pathways
  2. Cell Cycle/DNA Damage
  3. CDK

CDK

Cyclin dependent kinase

CDKs (Cyclin-dependent kinases) are serine-threonine kinases first discovered for their role in regulating the cell cycle. They are also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells. CDKs are relatively small proteins, with molecular weights ranging from 34 to 40 kDa, and contain little more than the kinase domain. In fact, yeast cells can proliferate normally when their CDK gene has been replaced with the homologous human gene. By definition, a CDK binds a regulatory protein called a cyclin. Without cyclin, CDK has little kinase activity; only the cyclin-CDK complex is an active kinase.

There are around 20 Cyclin-dependent kinases (CDK1-20) known till date. CDK1, 4 and 5 are involved in cell cycle, and CDK 7, 8, 9 and 11 are associated with transcription.

CDK levels remain relatively constant throughout the cell cycle and most regulation is post-translational. Most knowledge of CDK structure and function is based on CDKs of S. pombe (Cdc2), S. cerevisia (CDC28), and vertebrates (CDC2 and CDK2). The four major mechanisms of CDK regulation are cyclin binding, CAK phosphorylation, regulatory inhibitory phosphorylation, and binding of CDK inhibitory subunits (CKIs).

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-18930
    NU6300
    Inhibitor 98.44%
    NU6300 is a covalent, irreversible and ATP-competitive CDK2 inhibitor with an IC50 value of 0.16 μM. NU6300 can be used for the research of eukaryotic cell cycle- and transcription-related.
    NU6300
  • HY-145669
    DIF-3
    Inhibitor 99.84%
    DIF-3 is an orally active anticancer agent. DIF-3 reduces the expression levels of cyclin D1 and c-Myc by facilitating their degradation via activation of GSK-3β. DIF-3 inhibits Wnt/β-catenin signaling pathway-related proteins in cells. DIF-3 induces reactive oxygen species (ROS) and autophagy. DIF suppresses the growth of Trypanosoma. cruzi in HT1080 cells. DIF-3 exerts antitumor effects both in vitro and in vivo.
    DIF-3
  • HY-11009
    CGP60474
    Inhibitor 98.90%
    CGP60474, a highly potent anti-endotoxemic agent, is a potent cyclin-dependent kinase (CDK) inhibitor (IC50 values are 26, 3, 4, 216, 10, 200 and 13 nM for CDK1/B, CDK2/E, CDK2/A, CDK4/D, CDK5/p25, CDK7/H and CDK9/T, respectively). CGP60474 is a selective and ATP-competitive PKC inhibitor.
    CGP60474
  • HY-138946
    XY028-140
    Inhibitor 98.52%
    XY028-140 is a PROTAC connected by ligands for Cereblon and CDK. XY028-140 inhibits both CDK4/6 expression and CDK4/6 activity in cancer cells.
    XY028-140
  • HY-127104
    FMF-04-159-2
    Inhibitor 99.48%
    FMF-04-159-2 is a covalent CDK14 inhibitor. FMF-04-159-2 inhibits CDK14 and CDK2 with IC50s of 39.6 nM and 256 nM in NanoBRET assay, respectively.
    FMF-04-159-2
  • HY-111556
    BSJ-03-123
    Inhibitor 98.12%
    BSJ-03-123 is a PROTAC connected by ligands for Cereblon and CDK as a potent and novel CDK6-selective small-molecule degrader.
    BSJ-03-123
  • HY-N0417
    Cucurbitacin E
    Inhibitor 99.92%
    Cucurbitacin E is a natural compound which from Cucurbitaceae plants. Cucurbitacin E significantly suppresses the activity of the cyclin B1/CDC2 complex.
    Cucurbitacin E
  • HY-80013A
    THZ1 Hydrochloride
    Inhibitor 99.06%
    THZ1 Hydrochloride is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM. THZ1 Hydrochloride also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression.
    THZ1 Hydrochloride
  • HY-19984
    CCT-251921
    Inhibitor 99.01%
    CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor with an IC50 of 2.3 nM.
    CCT-251921
  • HY-N0815
    Resibufogenin
    Modulator 99.93%
    Resibufogenin is an orally active anticancer agent. Resibufogenin can be extracted from toad venom. Resibufogenin blocks signaling pathways such as PI3K/Akt, NF-κB, AP-1, activates GSK-3β, and regulates cyclin D1. Resibufogenin can activate central neurons. Resibufogenin has anti-inflammatory activity. Resibufogenin has anti-tumor effects on a variety of tumors such as multiple myeloma, renal cancer, colorectal cancer, pancreatic cancer, and glioma.
    Resibufogenin
  • HY-15004
    AUZ 454
    Inhibitor 99.15%
    AUZ 454 (K03861) is a type II CDK2 inhibitor with Kd of 8.2 nM. AUZ 454 (K03861) inhibits CDK2 activity by competing with binding of activating cyclins.
    AUZ 454
  • HY-15681
    Senexin A
    Inhibitor 99.79%
    Senexin A is an inhibitor of CDK8/19 (IC50: 280 nM, CDK8) and an inhibitor downstream of p21 transcription. It only inhibits p21-induced transcription but does not inhibit other biological effects of p21. Senexin A inhibits CMV-GFP induction as well as the p21 stimulatory activity of the consensus NF-κB-dependent promoters.
    Senexin A
  • HY-10014
    R547
    Inhibitor 99.57%
    R547 is a potent, selective and orally active ATP-competitive CDK inhibitor, with Kis of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively.
    R547
  • HY-112296
    T025
    Inhibitor 99.64%
    T025 is an orally active and highly potent inhibitor of Cdc2-like kinase (CLKs), with Kd values of 4.8, 0.096, 6.5, 0.61, 0.074, 1.5 and 32 nM for CLK1, CLK2, CLK3, CLK4, DYRK1A, DYRK1B and DYRK2, respectively. T025 induces caspase-3/7-mediated cell apoptosis. T025 reduces CLK-dependent phosphorylation. T025 exerts anti-proliferative activities in both hematological and solid cancer cell lines (IC50 values: 30-300 nM). T025 has an anti-tumor efficiency, mainly for MYC-driven disease research.
    T025
  • HY-W010128
    6-(Dimethylamino)purine
    Inhibitor 99.90%
    6-(Dimethylamino) purine (6-Dimethylaminopurine) is a serine threonine protein kinase inhibitor. 6-(Dimethylamino) purine can inhibit prolactin induced expression of lactoprotein genes in rabbit mammary gland cells. 6-(Dimethylamino) purine can affect the maturation of mammalian oocytes. 6-(Dimethylamino) purine can lead to downregulation of genes related to cell proliferation and cell cycle progression, such as proliferating cell nuclear antigen, insulin-like gene 1, and serine protease inhibitor 2 genes, and induce apoptosis in lymphoma cells (apoptosis).
    6-(Dimethylamino)purine
  • HY-144875
    CTX-712
    Inhibitor 98.15%
    CTX-712 is an orally effective CLK 2 inhibitor, with an IC50 of 1.4 nM, showing anti-tumor activity.
    CTX-712
  • HY-101800
    Senexin B
    Inhibitor 99.09%
    Senexin B (SNX2-1-165; BCD-115) is a potent, highly water-soluble and bioavailable CDK8/19 inhibitor, with Kds of 140 nM for CDK8 and 80 nM for CDK19.
    Senexin B
  • HY-13461A
    PHA-767491 hydrochloride
    Inhibitor 99.49%
    PHA-767491 hydrochloride is a dual Cdc7/Cdk9 inhibitor, with IC50s of 10 nM and 34 nM, respectively.
    PHA-767491 hydrochloride
  • HY-18299A
    Purvalanol A
    Inhibitor 98.30%
    Purvalanol A is a potent CDK inhibitor, which inhibits cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, cdk4-cyclin D1, and cdk5-p35 with IC50s of 4, 70, 35, 850, 75 nM, resepctively.
    Purvalanol A
  • HY-15878
    LDC000067
    Inhibitor 99.00%
    LDC000067 is a highly specific CDK9 inhibitor with an IC50 value of 44±10 nM in vitro.
    LDC000067
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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